Recent Developments in C−H Functionalization and Annulation of 2‐Aryl‐Quinazolinones and 3‐Aryl‐Quinazolinones <i>via</i> Site Selective Transformations

Abstract Quinazolinone is a crucial scaffold in numerous natural compounds, as well as in biologically active and functional materials. Consequently, various synthetic methods have been developed to transform quinazolinone and its derivatives. Site selective C−H bond functionalization and annulation of the 2‐aryl‐quinazolinones and 3‐aryl‐quinazolinones skeleton through transition‐metal catalysis offer an efficient approach to obtain diverse substituted nitrogen‐containing heterocyclic frameworks. This review summarizes recent reports on transition‐metal catalyzed site selective transformations of 2‐aryl‐quinazolinone and 3‐aryl‐quinazolinones through C−H functionalization and annulation reactions.